2-hydroxy-3-benzyl-5,6,7,8-tetrahydro quinoxaline | 113957-42-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2-hydroxy-3-benzyl-5,6,7,8-tetrahydro quinoxaline
• 英文别名: 2-hydroxy-3-benzyl-5,6,7,8-tetrahydroquinoxaline；3-Benzyl-5,6,7,8-tetrahydroquinoxalin-2(1H)-one；3-benzyl-5,6,7,8-tetrahydro-1H-quinoxalin-2-one
• CAS: 113957-42-9
• 化学式: C₁₅H₁₆N₂O
• 分子量: 240.305
• InChiKey: VKJBAVFUYDQLRZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  41.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-hydroxy-3-benzyl-5,6,7,8-tetrahydro quinoxaline 、 氯乙酸甲酯 生成 Methyl 2-[(3-benzyl-5,6,7,8-tetrahydroquinoxalin-2-yl)oxy]acetate
  参考文献：
  名称：

  YASO, MASAO;SUZUKI, YUKIO;SHIBATA, KENSUKE;MOCHIZUKI, DAISUKE;HAYASHI, EI+

  摘要：

  DOI：
• 作为产物：
  描述：

  alpha-氨基-苯丙酰胺盐酸盐(1:1) 、 1,2-环己二酮 在 盐酸 、 sodium hydroxide 、 碳酸氢钠 作用下， 以 甲醇 为溶剂， 生成 2-hydroxy-3-benzyl-5,6,7,8-tetrahydro quinoxaline
  参考文献：
  名称：

  1-substituted alkyl-1,2-dihydro-2-pyrazinone derivatives

  摘要：

  公式为## STR1 ##的1-取代烷基-1,2-二氢-2-吡嗪酮衍生物，其中A为低烷基; R.sub.1选择自烷基、苯基-低烷基和取代苯基-低烷基的群; R.sub.2和R.sub.3分别是低烷基，或者共同形成四亚甲基，R选择自羟基、卤素、低烷酰氧R.sub.4-氨基甲酸酯、芳基硫、1-甲基四氮唑-5-基硫、1-咪唑、吗啉、## STR2 ##其中R.sub.4是低烷基或芳基，R.sub.5是氢、低烷基或芳基，R.sub.6是氢、低烷基、羟基-低烷基、芳基、芳基-低烷酰基、芳基羰基、芳基磺酰基或噻吩基-低烷酰基，Ar是苯基或取代有C.sub.1-3烷基、卤素、硝基或低烷氧基的苯基，A、R.sub.1、R.sub.2和R.sub.3如上所定义，m为4-6的整数，n为2或3；以及其药学上可接受的盐。该化合物用作抑制血小板聚集、扩张血管和抗脂质过氧化物生成的药剂。

  公开号：

  US04837319A1

文献信息

• 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives
  申请人：Toyo Jozo Kabushiki Kaisha

  公开号：US04870176A1

  公开（公告）日：1989-09-26

  1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl; and R is selected from the group consisting of hydroxyl, halogen, lower alkanoyloxy, R.sub.4 -carbamoyloxy and arylthio, in which R.sub.4 is lower alkyl or aryl; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

  公式为##STR1##的1-取代烷基-1,2-二氢-2-吡嗪酮衍生物，其中A为低碳链；R.sub.1选自烷基、苯基-低碳基、和取代苯基-低碳基；R.sub.2和R.sub.3分别为低碳基；R选自羟基、卤素、低碳酰氧基、R.sub.4-氨基甲酸酯氧基和芳基硫基，其中R.sub.4为低碳基或芳基；以及其药学上可接受的盐。这些化合物可用作血小板聚集抑制剂、血管扩张剂和抗脂质过氧化生成剂。
• 1-substituted alkyl-2-oxo-hexahydroquinoxaline derivatives
  申请人：Toyo Jozo Kabushiki Kaisha

  公开号：US04877877A1

  公开（公告）日：1989-10-31

  1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of hydroxyl, halogen, lower alkanocyloxy, R.sub.4 -carbamoyloxy and arylthio, in which R.sub.4 is lower alkyl or aryl; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

  该文献描述了式子##STR1##的1-取代烷基-2-氧代-六氢喹诺啉衍生物，其中A是低碳链烷基；R.sub.1选自烷基、苯基-低碳链烷基和取代苯基-低碳链烷基；R选自羟基、卤素、低碳酰氧基、R.sub.4-氨基甲酸酯氧基和芳基硫醚，其中R.sub.4是低碳链烷基或芳基；以及其药学上可接受的盐。这些化合物可用作抑制血小板聚集、扩张血管和抗脂质过氧化产生的剂。
• 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives
  申请人：Toyo Jozo Kabushiki Kaisha

  公开号：US04877875A1

  公开（公告）日：1989-10-31

  1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of 1-methyltetrazole-5-yl-thio, 1-imidazolyl, morpholino, ##STR2## in which R.sub.5 is hydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A and R.sub.1 are as defined above, R.sub.2 and R.sub.3 are each lower alkyl or together form tetramethylene, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

  公式为##STR1##的1-取代烷基-2-氧代六氢喹喔啉衍生物，其中A为低碳烷基；R.sub.1选自烷基、苯基-低碳烷基和取代苯基-低碳烷基的群；R选自1-甲基四氮唑-5-基硫、1-咪唑基、吗啉、##STR2## 其中R.sub.5为氢、低碳烷基或芳基，R.sub.6为氢、低碳烷基、羟基-低碳烷基、芳基、芳基-低碳酰基、芳基羰基、芳基磺酰基或噻吩基-低碳酰基，Ar为苯基或取代有C.sub.1-3烷基、卤素、硝基或低碳烷氧基的苯基，A和R.sub.1如上定义，R.sub.2和R.sub.3各自为低碳烷基或一起形成四亚甲基，m为4-6的整数，n为2或3；以及其药学上可接受的盐。该化合物可用作抑制血小板聚集、扩张血管和抗脂质过氧化物生成的剂。
• 2-substituted alkoxy-3-substituted-pyrazines
  申请人：Toyo Jozo Kabushiki Kaisha

  公开号：US04894453A1

  公开（公告）日：1990-01-16

  A compound of the formula ##STR1## wherein Q is --CO-- or --CH.sub.2 --, R is hydroxyl, lower alkoxy, halogen, --NH-lower alkylene-OH, --NH-lower alkylene-arylthio, --NH-lower alkylene-halogen, ##STR2## in which ##STR3## is dilower alkylamino, cycloalkylamino, morpholino, ##STR4## in which R.sub.9 is hydrogen, lower alkyl or aryl, R.sub.10 is hydrogen, lower alkyl, hydroxy-lower alkyl, hydroxy-lower alkoxy-lower alkyl or di(aryl)-lower alkyl, m is an integer from 4 to 6, n is 2 or 3, R.sub.1 is alkyl or aryl-lower alkyl, R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene, and R.sub.4 is hydrogen, lower alkyl or aryl, in which aryl is phenyl which is optionally substituted with a group selected from the group consisting of 1-3 halogen, nitro, lower alkyl and lower alkoxy, or a pharmaceutically acceptable salt thereof, inhibits blood platelet aggregation, has vasodilating activity and inhibits lipoperoxide generation.

  化合物的化学式为 ##STR1## 其中Q为--CO--或--CH.sub.2 --，R为羟基，低烷氧基，卤素，--NH-低烷基-羟基，--NH-低烷基-芳基硫，--NH-低烷基-卤素，##STR2## 其中##STR3##为二低烷基氨基，环烷基氨基，吗啡基，##STR4##其中R.sub.9为氢，低烷基或芳基，R.sub.10为氢，低烷基，羟基-低烷基，羟基-低烷氧基-低烷基或二（芳基）-低烷基，m为4至6的整数，n为2或3，R.sub.1为烷基或芳基-低烷基，R.sub.2和R.sub.3分别为低烷基，或一起形成四亚甲基，R.sub.4为氢，低烷基或芳基，其中芳基为苯基，可选地用选自由1-3卤素，硝基，低烷基和低烷氧基的基团取代，或其药学上可接受的盐，抑制血小板聚集，具有扩血管作用并抑制脂质过氧化物生成。
• 1-Substituted Alkyl-1, 2-Dihydro-2-Pyrazinone derivatives
  申请人：TOYO JOZO KABUSHIKI KAISHA

  公开号：EP0242957A1

  公开（公告）日：1987-10-28

  Compounds of formula (I) wherein R is hydroxyl, halogen, lower alkanoyloxy, R4-carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazolyl, morpholino, or in which R4 is lower alkyl or aryl, Rs is hydrogen, lower alkyl or aryl, R6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, A and A, are lower alkylene, m is an integer of from 4 to 6, n is the integer 2 or 3; R, is alkyl aryl-lower alkyl or aryl; and R2 and R3 are each lower alkyl or together constitute tetramethylene; and pharmacologically acceptable non-toxic salts thereof; wherein aryl means phenyl unsubstututed or substituted by C1-3 alkyl, halogen, nitro or lower alkoxyl; have an inhibitory action on platelet aggregation, vasodilating activity and/or inhibitory action on lipoperoxide generation.

  式(I)化合物 其中 R 是羟基、卤素、低级烷酰氧基、R4-氨基甲酰氧基、芳硫基、1-甲基四唑-5-硫基、1-咪唑基、吗啉基、 或 其中 R4 是低级烷基或芳基，Rs 是氢、低级烷基或芳基，R6 是氢、低级烷基、羟基-低级烷基、芳基、芳基-低级烷酰基、芳基羰基、芳基磺酰基或噻吩基-低级烷酰基，A 和 A，是低级亚烷基，m 是 4 到 6 的整数，n 是 2 或 3 的整数；R，是烷基芳基-低级烷基或芳基；以及 R2 和 R3 分别为低级烷基或共同构成四亚甲基；及其药理上可接受的无毒盐；其中芳基指未被 C1-3 烷基、卤素、硝基或低级烷氧基取代或取代的苯基；具有抑制血小板聚集的作用、血管扩张活性和/或抑制脂过氧化物生成的作用。